IL192081A0 - Novel, cyclic substituted furopyrimidine derivatives and use thereof for treating cardiovascular diseases - Google Patents
Novel, cyclic substituted furopyrimidine derivatives and use thereof for treating cardiovascular diseasesInfo
- Publication number
- IL192081A0 IL192081A0 IL192081A IL19208108A IL192081A0 IL 192081 A0 IL192081 A0 IL 192081A0 IL 192081 A IL192081 A IL 192081A IL 19208108 A IL19208108 A IL 19208108A IL 192081 A0 IL192081 A0 IL 192081A0
- Authority
- IL
- Israel
- Prior art keywords
- alkyl
- alkoxy
- mono
- ocf
- cycloalkyl
- Prior art date
Links
- JUQAECQBUNODQP-UHFFFAOYSA-N furo[3,2-d]pyrimidine Chemical class C1=NC=C2OC=CC2=N1 JUQAECQBUNODQP-UHFFFAOYSA-N 0.000 title abstract 3
- 208000024172 Cardiovascular disease Diseases 0.000 title 1
- 125000004122 cyclic group Chemical group 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 12
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 102000009079 Epoprostenol Receptors Human genes 0.000 abstract 2
- 108091006335 Prostaglandin I receptors Proteins 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- -1 1H-tetrazol-5-yl Chemical group 0.000 abstract 1
- CBIWCJGTVQGGIQ-UHFFFAOYSA-N 2-[3-[[5-(4-methoxyphenyl)-6-phenylfuro[2,3-d]pyrimidin-4-yl]amino]phenoxy]acetic acid Chemical compound C1=CC(OC)=CC=C1C1=C(C=2C=CC=CC=2)OC2=NC=NC(NC=3C=C(OCC(O)=O)C=CC=3)=C12 CBIWCJGTVQGGIQ-UHFFFAOYSA-N 0.000 abstract 1
- 208000001953 Hypotension Diseases 0.000 abstract 1
- 239000012190 activator Substances 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 230000003257 anti-anginal effect Effects 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 230000001966 cerebroprotective effect Effects 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 230000002439 hemostatic effect Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000021822 hypotensive Diseases 0.000 abstract 1
- 230000001077 hypotensive effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000001525 receptor binding assay Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Furopyrimidine derivatives (I) are new. Furopyrimidine derivatives of formula (I) and their salts and solvates are new. A : O, S or NR 4>; R 4>H, 1-6C alkyl, 3-7C cycloalkyl or 4-7C cycloalkenyl; L 1>a bond or 1-4C alkanediyl; Q : 3-7C cycloalkyl, 5- to 7-membered heterocyclyl, phenyl or 5- or 6-membered heteroaryl, all optionally substituted with 1-2 of F, Cl, 1-4C alkyl, CF 3, OH, 1-4C alkoxy, OCF 3, NH 2 or mono- or di(1-4C alkyl)amino, where alkyl is optionally substituted with OH, 1-4C alkoxy, NH 2 or mono- or di(1-4C alkyl)amino; L 2>1-4C alkanediyl optionally mono- or disubstituted with F and optionally with one CH 2 group replaced by O or NR 5>; or 2-4C alkenediyl; R 5>H, 1-6C alkyl or 3-7C cycloalkyl; Z : COOR 7>, COCOOR 7>, 1H-tetrazol-5-yl or 5(4H)-oxo-1,3,4-oxadiazol-2-yl; R 7>H or 1-4C alkyl; R 1>, R 2>halo, CN, NO 2, 1-6C alkyl, 2-6C alkenyl, 2-4C alkynyl, 3-7C cycloalkyl, 4-7C cycloalkenyl, 1-6C alkoxy, CF 3, OCF 3, 1-6C alkylthio, 1-6C acyl, NH 2, mono- or di(1-6C alkyl)amino or 1-6C acylamino, where alkyl and alkoxy are optionally substituted with OH, 1-4C alkoxy, NH 2 or mono- or di(1-4C alkyl)amino, or an adjacent pair of R 1> and/or R 2> can form OCH 2O, OCHFO, OCF 2O, OCH 2CH 2O or OCF 2CF 2O; n, o : 0-3; R 3>H, 1-4C alkyl or cyclopropyl. An independent claim is also included for a process for preparing (I). [Image] ACTIVITY : Antianginal; Hypotensive; Cardiant; Anticoagulant; Cerebroprotective; Hemostatic; Vasotropic. MECHANISM OF ACTION : Prostacyclin receptor activator. 3-(5-(4-Methoxyphenyl)-6-phenylfuro[2,3-d]pyrimidin-4-ylamino)phenoxyacetic acid had an IC50 of 18 nM in a prostacyclin receptor binding assay.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005061171A DE102005061171A1 (en) | 2005-12-21 | 2005-12-21 | New furopyrimidine derivatives useful for treating cardiovascular diseases |
| PCT/EP2006/011825 WO2007079861A1 (en) | 2005-12-21 | 2006-12-08 | Novel, cyclic substituted furopyrimidine derivatives and use thereof for treating cardiovascular diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL192081A0 true IL192081A0 (en) | 2008-12-29 |
Family
ID=37758644
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL192081A IL192081A0 (en) | 2005-12-21 | 2008-06-12 | Novel, cyclic substituted furopyrimidine derivatives and use thereof for treating cardiovascular diseases |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8324222B2 (en) |
| EP (1) | EP1966218B1 (en) |
| JP (1) | JP2009523711A (en) |
| KR (1) | KR20080081325A (en) |
| CN (1) | CN101384602A (en) |
| AT (1) | ATE473982T1 (en) |
| AU (1) | AU2006334855A1 (en) |
| BR (1) | BRPI0620647A2 (en) |
| CA (1) | CA2633698A1 (en) |
| DE (2) | DE102005061171A1 (en) |
| ES (1) | ES2347593T3 (en) |
| IL (1) | IL192081A0 (en) |
| RU (1) | RU2008129364A (en) |
| WO (1) | WO2007079861A1 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102007019690A1 (en) * | 2007-04-26 | 2008-10-30 | Bayer Healthcare Ag | Use of cyclic substituted furopyrimidine derivatives for the treatment of pulmonary arterial hypertension |
| DE102007027800A1 (en) * | 2007-06-16 | 2008-12-18 | Bayer Healthcare Ag | Substituted bicyclic heteroaryl compounds and their use |
| DE102007051762A1 (en) | 2007-10-30 | 2009-05-07 | Bayer Healthcare Ag | Substituted pyrrolotriazines and their use |
| DE102007054786A1 (en) * | 2007-11-16 | 2009-05-20 | Bayer Healthcare Ag | Trisubstituted Furopyrimidines and their Use |
| JP5416774B2 (en) * | 2008-08-25 | 2014-02-12 | デュポン・エレクトロニック・ポリマーズ・エル・ピー | Novel propanoate and its production method |
| WO2022119823A1 (en) * | 2020-12-04 | 2022-06-09 | The Johns Hopkins University | Compounds and their use for treating neuropathic pain |
| CN115462369B (en) * | 2022-09-29 | 2023-09-22 | 安徽省立医院(中国科学技术大学附属第一医院) | A method for preserving vitrified exosomes |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3577420A (en) | 1968-01-05 | 1971-05-04 | Pfizer | Certain 4-aminofuro(2,3-d)pyrimidines |
| EP1018514B1 (en) | 1998-07-22 | 2004-05-12 | Daiichi Suntory Pharma Co., Ltd. | NF-$g(k)B INHIBITORS CONTAINING INDAN DERIVATIVES AS THE ACTIVE INGREDIENT |
| WO2000075145A1 (en) | 1999-06-03 | 2000-12-14 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| CA2350992C (en) | 1999-09-17 | 2009-06-23 | Suntory Limited | Preventive or therapeutic agents for myocarditis, dilated cardiomyopathy and heart failure comprising nf-kb inhibitors as active ingredients |
| DE60209721T2 (en) | 2001-05-14 | 2006-09-07 | Novartis Ag | OXAZOLO AND FUROPYRIMIDINES AND THEIR USE AS MEDICAMENTS AGAINST TUMORS |
| DE10141212A1 (en) | 2001-08-22 | 2003-03-06 | Bayer Ag | New 4-aminofuropyrimidines and their use |
| AU2002333524A1 (en) | 2001-09-11 | 2003-03-24 | Glaxosmithkline K.K. | Furo-and thienopyrimidine derivatives as angiogenesis inhibitors |
| DE10148883A1 (en) * | 2001-10-04 | 2003-04-10 | Merck Patent Gmbh | New fused bi- or tricyclic pyrimidine derivatives, are phosphodiesterase V inhibitors useful e.g. for treating impotence, cardiovascular disorders, inflammation or tumors |
| US20030225098A1 (en) * | 2002-03-21 | 2003-12-04 | Hirst Gavin C. | Kinase inhibitors |
| KR20050091462A (en) | 2004-03-12 | 2005-09-15 | 한국과학기술연구원 | Furopyrimidine compound and ddr2 tyrosine kinase activity inhibitor comprising the same |
| KR20070055486A (en) | 2004-06-10 | 2007-05-30 | 젠션 디스커버리 리미티드 | Puranopyrimidine Compounds Effective as Potassium Channel Inhibitors |
| US7776867B2 (en) | 2004-06-29 | 2010-08-17 | Amgen Inc. | Furanopyrimidines |
-
2005
- 2005-12-21 DE DE102005061171A patent/DE102005061171A1/en not_active Withdrawn
-
2006
- 2006-12-08 BR BRPI0620647-6A patent/BRPI0620647A2/en not_active IP Right Cessation
- 2006-12-08 KR KR1020087017645A patent/KR20080081325A/en not_active Withdrawn
- 2006-12-08 WO PCT/EP2006/011825 patent/WO2007079861A1/en not_active Ceased
- 2006-12-08 CN CNA200680053205XA patent/CN101384602A/en active Pending
- 2006-12-08 CA CA002633698A patent/CA2633698A1/en not_active Abandoned
- 2006-12-08 ES ES06840964T patent/ES2347593T3/en active Active
- 2006-12-08 EP EP06840964A patent/EP1966218B1/en not_active Not-in-force
- 2006-12-08 DE DE502006007450T patent/DE502006007450D1/en active Active
- 2006-12-08 US US12/086,784 patent/US8324222B2/en not_active Expired - Fee Related
- 2006-12-08 RU RU2008129364/04A patent/RU2008129364A/en not_active Application Discontinuation
- 2006-12-08 AT AT06840964T patent/ATE473982T1/en active
- 2006-12-08 JP JP2008546192A patent/JP2009523711A/en active Pending
- 2006-12-08 AU AU2006334855A patent/AU2006334855A1/en not_active Abandoned
-
2008
- 2008-06-12 IL IL192081A patent/IL192081A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2347593T3 (en) | 2010-11-02 |
| US8324222B2 (en) | 2012-12-04 |
| US20110124665A1 (en) | 2011-05-26 |
| CN101384602A (en) | 2009-03-11 |
| KR20080081325A (en) | 2008-09-09 |
| WO2007079861A1 (en) | 2007-07-19 |
| EP1966218A1 (en) | 2008-09-10 |
| RU2008129364A (en) | 2010-01-27 |
| AU2006334855A1 (en) | 2007-07-19 |
| EP1966218B1 (en) | 2010-07-14 |
| DE102005061171A1 (en) | 2007-07-05 |
| DE502006007450D1 (en) | 2010-08-26 |
| ATE473982T1 (en) | 2010-07-15 |
| BRPI0620647A2 (en) | 2011-11-16 |
| JP2009523711A (en) | 2009-06-25 |
| CA2633698A1 (en) | 2007-07-19 |
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